Abstract

SYNTHESIS, CHARACTERIZATION ANDINVITRO CYTOTOXIC EVALUATION OF NOVEL AMIDE DERIVATIVES OF 5-[2-(4- METHOXYPHENYL)PYRIDIN-3-YL]-1, 3, 4-THIADIAZOL-2-AMINE.

Adimule Vinayak, Medapa Sudha, Kumar S lalita, RaoPrakash Kumar

Abstract

In this research we have synthesized five novel amide derivatives of 5- [2-(4-methoxyphenyl) pyridin-3-yl]-1, 3, 4-thiadiazol-2-amine and evaluated their cytotoxicity by MTT assay. Three cell lines were used for the evaluation HeLa, HepG2 and PANC-1. All the synthesized compounds were characterized by LCMS, IR, 1H and 13C (proton and Carbon 13) spectroscopies and elemental analysis. These compounds were evaluated for invitro anticancer activity on three different human leukemic cell lines, namely HeLa, HepG2 and PANC-1.In total five compounds were synthesized and studied for their MTT assay. Among five synthesized novel compounds, the compound 2-chloro-N-{5-[2- (4-methoxyphenyl)pyridin-3-yl]-1, 3, 4-thiadiazol-2-yl} pyridine-3- carboxamide6d is highly cytotoxic on HeLa and PANC-1 cell lines having IC50 of 2.8μM and 1.8 μM respectively. Rest all the compound showed less cytotoxicity on all the three cell lines as compared with the standard 5-FU1.

Keywords: HeLa, 1, 3, 4-thidiazoles, Thiosemicarbazide, Anticancer, MTT assay.