ANTIPROLIFERATIVE AND IN SILICO ADMET STUDY OF NEW 4-(PIPERIDIN-1-YLMETHYL)-2- (THIOPHEN-2-YL) QUINOLINE ANALOGUES


Harishkumar S, Satyanarayan Nd, Santhosha Sm

Abstract


 Objective: Synthesis and antiproliferative study of novel 4-(piperidin-1-ylmethyl)-2-(thiophen-2-yl) quinoline 7(a-j) derivatives.

Methods: 4-(piperidin-1-ylmethyl)-2-(thiophen-2-yl) quinolines were synthesized by the addition of 4-(chloromethyl)-2-(thiophen-2-yl) quinoline (0.01 mol), piperidine (0.01 mol) in DMF (10 v) and K2CO3 (0.02 mol). The anticancer activity of the title compounds performed against T-47D, HeLa, HepG2, and MCF-7 human cancer cell lines growth was investigated by MTT assay.

Results: The compounds 7b and 7g exhibited 90% of the growth inhibitory effect on T-47D, HeLa, and MCF-7 and also 80% growth inhibition in HepG2 when compared with standard drug paclitaxel.

Conclusion: The synthesized compounds 4-(piperidin-1-ylmethyl)-2-(thiophen-2-yl) quinoline 7(a-j) exhibited a considerable degree of growth inhibition of human cancer cell lines. The synthesized molecules 7(a-j) are in acceptable range and are less toxic and can be considered as possible hits for drug discovery.


Keywords


MTT assay, In silico, T-47D, HeLa, HepG2, MCF-7, Molinspiration.

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About this article

Title

ANTIPROLIFERATIVE AND IN SILICO ADMET STUDY OF NEW 4-(PIPERIDIN-1-YLMETHYL)-2- (THIOPHEN-2-YL) QUINOLINE ANALOGUES

Keywords

MTT assay, In silico, T-47D, HeLa, HepG2, MCF-7, Molinspiration.

DOI

10.22159/ajpcr.2018.v11i4.24147

Date

01-04-2018

Additional Links

Manuscript Submission

Journal

Asian Journal of Pharmaceutical and Clinical Research
Vol 11 Issue 4 April 2018 Page: 306-313

Print ISSN

0974-2441

Online ISSN

2455-3891

Authors & Affiliations

Harishkumar S
Kuvempu University, Department of Pharmaceutical Chemistry, Post Graduate Centre, Kadur-577548
India

Satyanarayan Nd
Kuvempu University, Department of Pharmaceutical Chemistry, Post Graduate Centre, Kadur-577548
India

Santhosha Sm
Kuvempu University, Department of Pharmaceutical Chemistry, Post Graduate Centre, Kadur-577548
India


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