Synthesis of Novel Benzamide- piperazine-sulfonamide Hybrids as Potential Anticancer Agents

The synthesis of a series of substituted hippuric acid (2-benzamidoacetic acid) derivatives containing arylsulfonylpiperazine nucleus (3a-j, 4a-j) is described. The compounds were synthesized by coupling hippuric/4-fluorohippuric acid with various arylsulfonylpiperazines using N-(3-dimethylaminoprop...

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Bibliographic Details
Published in:Croatica Chemica Acta 2019, Vol.92 (3), p.1
Main Authors: Rao, B. Ramalingeswara, Katiki, Mohana Rao, Kommula, Dileep, Narayanan, Saishyam, Murty, M.S.R
Format: Article
Language:English
Subjects:
anticancer
Antineoplastic agents
arylsulfonylpiperazine
Cancer
Cancer treatment
EDCI
MTT assay
Skin
Sulfonamides
Third generation wireless technology
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Summary:The synthesis of a series of substituted hippuric acid (2-benzamidoacetic acid) derivatives containing arylsulfonylpiperazine nucleus (3a-j, 4a-j) is described. The compounds were synthesized by coupling hippuric/4-fluorohippuric acid with various arylsulfonylpiperazines using N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (EDCI). The structures of all the new compounds were confirmed by IR, NMR and MS spectral data. All the synthesized compounds have been evaluated for their in vitro cytotoxicity towards five human cancer cell lines of different origins viz. HeLa (Cervical), A549 (Lung), A375 (Skin), MD-AMB-231(Breast) and T98G (brain) and their [IC.sub.50] values were determined. Among the compounds tested, 3b, 3d, 3g, 4c and 4e displayed significant cytotoxic activity ([IC.sub.50] = 24.2-38.2 [micro]M). T98G was the most sensitive cell line towards the compounds studied followed by HeLa, A375, A549 and MD-AMB-231. Keywords: arylsulfonylpiperazine, EDCI, anticancer, MTT assay.
ISSN:0011-1643
1334-417X
DOI:10.5562/cca3535