Scribd Logo
Upload

Welcome to Scribd!

  • 29 views

    56 TH Ipc Abstract

    Uploaded by

    dinesh111180
    The document describes the synthesis of four novel L-glutamic acid analogs as potential anti-cancer agents. Specifically: 1) Benzenesulphonyl chloride was reacted with L-glutamic acid to obtain N-(benzenesulphonyl)-L-glutamic acid, which was then converted to the dichloride derivative. 2) p-Substituted phenylhydrazines were synthesized and reacted with the acid chloride to obtain the title compounds with p-H, CH3, Cl, and NO2 substituents. 3) The p-nitro analog exhibited the most potent anticancer activity in prostate cancer cell lines, comparable to adriamycin.

    Copyright:

    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd

    56 TH Ipc Abstract

    Uploaded by

    dinesh111180
    29 views2 pages
    The document describes the synthesis of four novel L-glutamic acid analogs as potential anti-cancer agents. Specifically: 1) Benzenesulphonyl chloride was reacted with L-glutamic acid to obtain N-(benzenesulphonyl)-L-glutamic acid, which was then converted to the dichloride derivative. 2) p-Substituted phenylhydrazines were synthesized and reacted with the acid chloride to obtain the title compounds with p-H, CH3, Cl, and NO2 substituents. 3) The p-nitro analog exhibited the most potent anticancer activity in prostate cancer cell lines, comparable to adriamycin.

    Original Description:

    ipc abstract of antiepileptic

    Original Title

    56 Th Ipc Abstract

    Copyright

    © © All Rights Reserved

    Available Formats

    PDF, TXT or read online from Scribd

    Did you find this document useful?

    Is this content inappropriate?

    The document describes the synthesis of four novel L-glutamic acid analogs as potential anti-cancer agents. Specifically: 1) Benzenesulphonyl chloride was reacted with L-glutamic acid to obtain N-(benzenesulphonyl)-L-glutamic acid, which was then converted to the dichloride derivative. 2) p-Substituted phenylhydrazines were synthesized and reacted with the acid chloride to obtain the title compounds with p-H, CH3, Cl, and NO2 substituents. 3) The p-nitro analog exhibited the most potent anticancer activity in prostate cancer cell lines, comparable to adriamycin.

    Copyright:

    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    29 views2 pages

    56 TH Ipc Abstract

    Uploaded by

    dinesh111180
    The document describes the synthesis of four novel L-glutamic acid analogs as potential anti-cancer agents. Specifically: 1) Benzenesulphonyl chloride was reacted with L-glutamic acid to obtain N-(benzenesulphonyl)-L-glutamic acid, which was then converted to the dichloride derivative. 2) p-Substituted phenylhydrazines were synthesized and reacted with the acid chloride to obtain the title compounds with p-H, CH3, Cl, and NO2 substituents. 3) The p-nitro analog exhibited the most potent anticancer activity in prostate cancer cell lines, comparable to adriamycin.

    Copyright:

    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    of 2

    Increased uptake of glutamic acid is observed in

    tumor cells due to increased metabolic activity. Hence


    B27 Studies On Some Novel Thieno[2,3-d]- agents that can interfere with the uptake, biosynthesis or
    functions of glutamic acid can act as antitumour agents.
    Pyrimidine: Part I. Synthesis &
    For example, L-glutamic acid analogs have been re-
    Antimicrobial Evaluation Of 4-Imino, 3- ported to have antitumour activity. Hydrazine moiety
    (Substituted Benzothiazole-2-Yl), 5,6, showed potential for improving anticancer and
    Disubstituted Thieno (2,3-d) Pyrimidine anticachexia activity. In the present work the synthesis of
    2(1H)- Thiones. four novel glutamic acid analogs with structure N-
    (benzenesulphonyl)-L-glutamic acid bis-( substituted
    Laddha SS1, Patil SG1, Surana SJ*1, Ganguly S2, & phenylhydrazides) are reported. The substituents on the
    Bhatnagar SP2 phenyl hydrazide moiety are p-H, NO2, Cl & CH3.
    1 Medicinal Chemistry Division, R. C. Patel College of i)Benzenesulphonyl chloride was condensed with
    Pharmacy, Shirpur, Dist: Dhule. L-glutamic acid in basic medium to obtain N-
    2 Dept. of Pharmaceutical Sciences, Birla Institute of (benzenesulphonyl)-L-glutamic acid. Dry N-
    Technology, Mesra, Ranchi. (benzenesulphonyl)-L-glutamic acid was converted to N-
    (benzenesulphonyl)-L-glutamic acid dichloride by reflux-
    The clinical need for an antimicrobial has related ing with thionyl chloride. ii) Synthesis of p-substituted
    in series of papers appearing on the synthesis, prelimi- phenyl hydrazines involved diazotisation of p-substituted
    nary screening of various nitrogen heterocyclic systems, anilines using NaNO2 & HCl followed by reduction using
    especially pyrido (2,3-d) pyrimidine and thieno (2,3-d) sodium sulphite Alternatively the p-nitro isomer was pre-
    pyrimidine. pared by nucleophilic substitution of p-bromo nitroben-
    zene with hydrazine hydrate. The acid chloride of step (i)
    Numerous thieno (2,3-d) pyrimidines are known to was refluxed with p-substituted phenylhydrazines of step
    possess a broad spectrum of biological activities. Some (ii) in anhydrous THF to get N-(benzenesulphonyl)-L-
    of them are useful as antifolates, antihyperlipademic, glutamic acid bis-( substituted phenylhydrazides) having
    analgesics and antibacterial activity. Also many substituents like p-H, CH3, Cl & NO2 .
    benzothiazole derivatives have been found application
    as analgesics, anti-inflammatory and antibacterial. In view Anticancer activity was determined for the com-
    of these benefits and as a continuation of our work, the pounds in two prostate cancer cell lines (DU 145 & PC 3)
    present investigation was planned to synthesize novel 4- by using MTT assay. Adriamycin was used as the
    imino, 3-(substituted benzothiazole-2-yl), 5,6, disubsti- standrard for the comparison. Out of four compounds,
    tuted thieno (2,3-d) pyrimidine 2(1H)-thiones in the hope the p-nitro isomer exhibited potent anticancer activity and
    of obtaining compounds with both thieno (2,3-d) pyrimi- in cell line DU 145 its activity (84.7 %) is comparable to
    dine and benzothiazole nucleus in a single framework adriamycin (86.6%) at 80 µg/ml. Also in PC-3, it showed
    with enhanced biological and medicinal properties. 72.0 % inhibition as compared to adriamycin (98.3%) at
    80 µg/ml.
    The starting compounds 3-cyano, 2-amino, 4,5-dis-
    ubstituted thiophen (Gewalds) has been prepared by re-
    ported method. Gewald was treated with CS2 in dry pyri-
    dine using the known method gives 4-imino, 5,6, disub-
    B29 Synthesis Of P-Chlorophenyl
    stituted thieno (2,3-d) 1,3 thiazine-2-thione. 4-imino, 5,6, Semicarbazones As Potential
    disubstituted-thieno (2,3-d) 1,3 thiazine-2-thione on re- Anticonvulsants-And Their Effect On
    action with 2-amino benzothiazoles in the presence of Gaba Shunt
    dry pyridine yielded various derivatives of 4-imino, 3-(sub-
    stituted benzothiazole-2-yl), 5,6, disubstituted thieno (2,3- S.K.Patnaik, S.N.Pandeya, S.V.Chaudhari, N.Mahajan,
    d) pyrimidine 2(1H)-thiones. The structure of the final D.Thakkar*
    compound was derived from Elemental analysis and
    Department of Pharmaceutics, Institute of Technology,
    spectral studies (IR, NMR).
    Banaras Hindu University, Varanasi - 221 005
    The title compounds were tested for their Antimi-
    Anticonvulsant drugs selectively depress the cen-
    crobial activity and several of the title product shows prom-
    tral nervous system and are used in the treatment of Epi-
    ising antibacterial activity against both Gram positive and
    lepsy. The past few decades, experienced a great variety
    Gram negative bacteria.
    of chemical compounds have been tried for the cure of
    epileptic seizures.

    B28 Synthesis and Evaluation of L-Glutamic Various compounds related to semicarbazone,


    Acid Analogs as Potential Anti-Cancer thiosemicarbazones and hydrazones were designed and
    synthesized with the aim to develop newer anticonvulsants.
    Agents.
    Lokhande T. N.*, Viswanathan C. L. and Deb S.
    Bombay College of Pharmacy, Santacruz (E), Mumbai –98.

    56th IPC Kolkata - Scientific Oral Presentations - Medicinal Chemistry 39


    O PMR and Mass) data. The synthesis has been effected
    NH C
    NH
    Cl N
    S by making use of appropriate 2,4-dicarboethoxy-cyclo-
    N NH C
    Cl H 3C C S NH hexanone, formaldehyde and appropriate primary amines
    HC N
    OH ] by the bis-Mannich condensation reaction. The required
    3-aryl-2, 4-dicarboethoxy-5-hydroxy-5-methylcyc
    OH
    lohexanones have been also synthesized from appro-
    I II priate aldehydes and the ethylactoacetate by the MWI
    method as well as, for the first time. The synthesized
    Cl N S
    Cl
    O
    C
    H2
    C
    compound was screened for their analgesic,
    NH C
    S
    HC N
    NH NH antihistaminic, local anesthetic and anti-inflammatory
    HC N

    OH
    activities by standard methods. Some of the compounds
    found to exhibit good anti-inflammatory local anesthetic
    OCH 3 and antihistaminic activities, in comparison with the stan-
    dards employed.
    III IV

    1
    These compounds were characterized by UV, IR,
    H NMR spectral and elemental analysis. All the synthe-
    B32 Synthesis and Characterization of a b-
    sized compounds were screened for their anticonvulsant glucoside Conjugate of Doxorubicin
    activity against maximal electroshock seizures test, strych- for Application in ADEPT and/or PMT
    nine induced seizure method, and Metrazole induced D. H. Krishna*, D. R. Krishna, N.Raghavender,
    seizure method in which all the compounds were found Y.Venkateshwarlu, C. E. Mueller, A.R.Rao.
    to have anticonvulsant activity.
    Anthracycline antibiotics, particularly doxorubicin
    Further, the compounds were evaluated for their and daunorubicin, have been used extensively in the
    effect on GABA levels in various regions of brain in rat by treatment of human malignancies. However cardiotoxicity
    enzymatic UV and fluorimetric method, using clobazam and multidrug resistance are significant problems that
    as a standard drug. It was found that overall these com- limit the clinical efficacy of such agents. Rational design
    pounds increased the GABA levels in rat brain in the range to avoid these side effects includes strategies such as
    of 10% to 50% with maximum rise in cerebellum, while drug targeting and prodrug synthesis. Ideally, the activation
    the rise by clobazam was found to be 40%. The results of a prodrug should be restricted to the required site of
    show that among all synthesized compounds; compound action, the tumor cell.
    I,(4-(4’-chlorophenyl)-4-hydroxyacetophenone
    semicarbazone) was found to be more active than Clobazam. Several cancerous tissues and tumors are rich in
    certain lysosomal enzymes as compared to those found
    Thus it can be predicted that the anticonvulsant prop- in the normal tissues. Thus, a prodrug can be designed
    erty of the synthesized compounds might be due to their to selectively target such tumor cells where it can be
    influence of GABA mediated inhibition and the chloro sub- activated to antineoplastic agent. This approach protects
    stituent at position para to the semicarbazone along with the normal cells from the cytotoxic effects of the drug. In
    NH-CO-NH-N= linkage is essential for their potential this context, a large number of prodrugs have recently
    anticonvulsant activity. been developed that can be transformed into active
    anticancer drugs by enzymes of both mammalian and
    nonmammalian origin. However, further investigations
    B31 Rapid one-Pot Microwave-assisted were not undertaken to introduce these prodrugs for
    Double Mannich Condensation of clinical use.
    Polysubstituted Cyclohexanones and In this regard, the combination of prodrugs with tu-
    Pharmacological Activities of Their mor-specific enzymes for use as therapeutic agents was
    Derivatives reported by Connors and re-emphasized in the case of an-
    titumor drugs by Bagshawe and Senter, who termed the
    Navanath Kalyane*, B. Shivakumar and V.M.Reddy**
    approach “antibody-directed enzyme prodrug therapy
    1 Karnataka College of Pharmacy PO Box 53, Bidar. (ADEPT)”. In this strategy, the antibody-enzyme conjugate is
    2 Dr. Ch. Ravi Shankar Memorial Medicinal Chemistry first injected and localized at the tumor cell surface antigen.
    Research Laboratory, University College of Pharma- Subsequently, the nontoxic prodrug is administered , and
    ceutical Sciences, Kakatiya University, Warangal. the cytotoxic species is released on the tumor cell surface.
    In view of growing pharmacological importance of We present here a doxorubicin prodrug (1) that is
    azabicyclononanes and their synthesis a more facile, rapid activated by b-glucosidase.The approach is based on
    one-pot and microwave irradiation method has been stud- the use of certain para-substituted benzyloxycarbonyl
    ied for their synthesis and compared with the conven- groups as bioreversible amine protecting agents. These
    tional one, in the present investigation. As many as thirty agents function as a spacer between glucose and
    new substituted 8-aryl-3-alkyl/aralkyl/aryl/-azabicyclo anthracycline moieties. Only after enzymatic cleavage did
    [3.3.1] nonanes have been synthesized, purified and char- spontaneous self decomposition of this spacer occur to
    acterized with the help of their analytical and spectral (IR, release the drug (3).

    40 56th IPC Kolkata - Scientific Oral Presentations - Medicinal Chemistry

    You might also like