2. Academic Validation
  3. Synthesis and evaluation of novel sulfonamide analogues of 6/7-aminoflavones as anticancer agents via topoisomerase II inhibition

Synthesis and evaluation of novel sulfonamide analogues of 6/7-aminoflavones as anticancer agents via topoisomerase II inhibition

  • Bioorg Med Chem Lett. 2020 Jul 15;30(14):127246. doi: 10.1016/j.bmcl.2020.127246.
Rohini N Shelke 1,  Dattatraya N Pansare 2,  Aniket P Sarkate 3,  Ishudeep K Narula 3,  Deepak K Lokwani 4,  Shailee V Tiwari 5,  Rajaram Azad 6,  Shankar R Thopate 7
Affiliations

Affiliations

  • 1 Department of Chemistry, Prof John Barnabas Post Graduate School of Biological Studies, Ahmednagar College, Ahmednagar, Ahmednagar 414001, India.
  • 2 Department of Chemistry, Deogiri College, Station Road, Aurangabad 431 005, MS, India.
  • 3 Department of Chemical Technology, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad 431 004, MS, India.
  • 4 Department of Pharmaceutical Chemistry, R C Patel Institute of Pharmaceutical Education & Research, Shirpur 425405, MS, India.
  • 5 Department of Pharmaceutical Chemistry, Durgamata Institute of Pharmacy, Dharmapuri, Parbhani 431401, MS, India.
  • 6 Department of Animal Biology, University of Hyderabad, Hyderabad, 500046, India.
  • 7 Department of Chemistry, Prof John Barnabas Post Graduate School of Biological Studies, Ahmednagar College, Ahmednagar, Ahmednagar 414001, India. Electronic address: srthopate@gmail.com.
PMID: 32527548 DOI: 10.1016/j.bmcl.2020.127246
Abstract

A series of new sulfonamide analogues of 6/7-aminoflavones were synthesized by using molecular hybridization approach. These new sulfonamide analogues were screened for antiproliferative activity against human hepatocellular carcinoma (HepG-2), human lung Cancer cell line (A-549), human colorectal adenocarcinoma (Caco-2) Cancer cell lines. Compounds 5p, 5q, 5t, 5v, 5w and 5x exhibited good Anticancer activity against selected Cancer cell lines. These compounds were further evaluated to predict their ability to inhibit topoisomerase-II enzyme. Compound 5x has shown potent antiproliferative activity (IC50 value 0.98 µM) as compared to standard drug Adriamycin (IC50 = 0.94 µM) indicating that these compounds exhibits Anticancer activity via inhibition of topoisomerase-II enzyme. Docking results also have supported above observations by indicating that compounds are held in the active pocket by combination of various hydrogen and hydrophobic interactions with Top II-DNA-etoposide enzyme.

Keywords

Aminoflavones; Anticancer activity; Docking; Sulfonamide; topoisomerase-II.

Figures
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z