Antiproliferative and tumor inhibitory studies of 2,3 disubstituted 4-thiazolidinone derivatives

被引：52

作者：

Kumar, Kothanahally S. Sharath ^{[1
]}

Hanumappa, Ananda ^{[1
]}

Vetrivel, Maruthai ^{[2
]}

Hegde, Mahesh ^{[1
]}

Girish, Yarabhally R. ^{[1
]}

Byregowda, Thinnali R. ^{[2
]}

Rao, Suguna ^{[2
]}

Raghavan, Sathees C. ^{[3
]}

Rangappa, Kanchugarakoppal S. ^{[1
]}

机构：

[1] Univ Mysore, Dept Studies Chem, Mysuru 570006, Karnataka, India

[2] Vet Coll, Dept Vet Pathol, Bengaluru 560024, Karnataka, India

[3] Indian Inst Sci, Dept Biochem, Bengaluru 560012, Karnataka, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2015年 / 25卷 / 17期

关键词：

4-Thiazolidinone; T3P; Reh; EAC; Tumor regression; BIOLOGICAL EVALUATION; EASY ACCESS; THIAZOLIDINONES; IDENTIFICATION; THIAZOLES; DISCOVERY; POTENT; AGENTS;

D O I：

10.1016/j.bmcl.2015.06.069

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

4-Thiazolidinone derivatives were synthesized using T3P (R)-DMSO media as a cyclodehydrating agent. All the molecules were tested for their cytotoxicity against leukemic cell lines. The compound 3-(4-bromophenyl)-2-(4-(dimethylamino)phenyl)thiazolidin-4-one (4e) with electron donating substituent at para position of phenyl ring displayed considerable cytotoxicity against Reh and Nalm6 cells with an IC50 value of 11.9 and 13.5 mu M, respectively. Furthermore, the compound 4e tested for tumor regression studies induced by EAC in Swiss albino mouse. Both in vitro and in vivo results suggested significant antiproliferative activity of compound 4e in Reh cells and mouse tumor tissue treated with compound 4e showed multifocal areas of necrosis and numerous number of apoptotic cells. (C) 2015 Elsevier Ltd. All rights reserved.

引用

页码：3616 / 3620

页数：5

共 30 条

[1] Synthesis and preliminary evaluation of some substituted coumarins as anticonvulsant agents
Amin, Kamelia M.
Rahman, Doaa E. Abdel
Al-Eryani, Yasmin A.
[J]. BIOORGANIC & MEDICINAL CHEMISTRY, 2008, 16 (10) : 5377 - 5388
[2] Synthesis, spectral and biological evaluation of some new thiazolidinones and thiazoles based on t-3-alkyl-r-2,c-6-diarylpiperidin-4-ones
Aridoss, G.
Amirthaganesan, S.
Kim, M. S.
Kim, J. T.
Jeong, Yeon Tae
[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2009, 44 (10) : 4199 - 4210
[3] Discovery of 2,3-diaryl-1,3-thiazolidin-4-ones as potent anti-HIV-1 agents
Barreca, ML
Chimirri, A
De Luca, L
Monforte, AM
Monforte, P
Rao, A
Zappalà, M
Balzarini, J
De Clercq, E
Pannecouque, C
Witvrouw, M
[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2001, 11 (13) : 1793 - 1796
[4] Design, Synthesis and Pharmacological Screening of Novel Antihypertensive Agents Using Hybrid Approach
Bhandari, Shashikant V.
Bothara, Kailash G.
Patil, Ajit A.
Chitre, Trupti S.
Sarkate, Aniket P.
Gore, Suraj T.
Dangre, Sudarshan C.
Khachane, Chetan V.
[J]. BIOORGANIC & MEDICINAL CHEMISTRY, 2009, 17 (01) : 390 - 400
[5] Chemical probes of UDP-galactopyranose mutase
Carlson, Erin E.
May, John F.
Kiessling, Laura L.
[J]. CHEMISTRY & BIOLOGY, 2006, 13 (08): : 825 - 837
[6] Photochemically enhanced binding of small molecules to the tumor necrosis factor receptor-1 inhibits the binding of TNF-α
Carter, PH
Scherle, PA
Muckelbauer, JA
Voss, ME
Liu, RQ
Thompson, LA
Tebben, AJ
Solomon, KA
Lo, YC
Li, Z
Strzemienski, P
Yang, GJ
Falahatpisheh, N
Xu, M
Wu, ZR
Farrow, NA
Ramnarayan, K
Wang, J
Rideout, D
Yalamoori, V
Domaille, P
Underwood, DJ
Trzaskos, JM
Friedman, SM
Newton, RC
Decicco, CP
[J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 2001, 98 (21) : 11879 - 11884
[7] Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors
Chen, Shaoqing
Chen, Li
Le, Nam T.
Zhao, Chunlin
Sidduri, Achyutharao
Lou, Jian Ping
Michoud, Christophe
Portland, Louis
Jackson, Nicole
Liu, Jin-Jun
Konzelmann, Fred
Chi, Feng
Tovar, Christian
Xiang, Qing
Chen, Yingsi
Wen, Yang
Vassilev, Lyubomir T.
[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2007, 17 (08) : 2134 - 2138
[8] Rhodanine derivatives as inhibitors of JS']JSP-1
Cutshall, NS
O'Day, C
Prezhdo, M
[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2005, 15 (14) : 3374 - 3379
[9] Discovery of small molecule integrin αvβ3 antagonists as novel anticancer agents
Dayam, Raveendra
Aiello, Francesca
Deng, Jinxia
Wu, Yun
Garofalo, Antonio
Chen, Xiaoyuan
Neamati, Nouri
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 2006, 49 (15) : 4526 - 4534
[10] Identification of small-molecule inhibitors of interaction between the BH3 domain and Bcl-xL
Degterev, A
Lugovskoy, A
Cardone, M
Mulley, B
Wagner, G
Mitchison, T
Yuan, JY
[J]. NATURE CELL BIOLOGY, 2001, 3 (02) : 173 - 182

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