Unknown

Dataset Information

0

D-Ring-Modified Analogues of Luotonin A with Reduced Planarity: Design, Synthesis, and Evaluation of Their Topoisomerase Inhibition-Associated Cytotoxicity.

ABSTRACT: A- and D-ring-modified luotonin-inspired heterocycles have been synthesized and were evaluated for their activity against the viability of four cancer cell lines in vitro, namely, MCF7, HCT116, JURKAT, and NCI-H460. The analysis of results indicated that two of the synthesized derivatives displayed good inhibition against the growth of the human colon cancer HCT116 cell line, with potencies lower than but in the same order of magnitude as camptothecin (CPT). These two luotonin analogues also showed an activity similar to that of the highly potent alkaloid CPT as inhibitors of topoisomerase I and also inhibited topoisomerase II. These results show that complete planarity is not a strict requirement for topoisomerase inhibition by luotonin-related compounds, paving the way to the design of analogues with improved solubility.

SUBMITTER: Almansour AI 

PROVIDER: S-EPMC6877907 | biostudies-literature | 2019

REPOSITORIES: biostudies-literature

Json Xml
altmetric image

Publications

D-Ring-Modified Analogues of Luotonin A with Reduced Planarity: Design, Synthesis, and Evaluation of Their Topoisomerase Inhibition-Associated Cytotoxicity.

Almansour Abdulrahman I AI   Kumar Raju Suresh RS   Arumugam Natarajan N   Bianchini Giulia G   Menéndez J Carlos JC   Mohammad Faruq F   Dupadahalli Kotresha K   Altaf Mohammad M  

BioMed research international 20191113

A- and D-ring-modified luotonin-inspired heterocycles have been synthesized and were evaluated for their activity against the viability of four cancer cell lines in vitro, namely, MCF7, HCT116, JURKAT, and NCI-H460. The analysis of results indicated that two of the synthesized derivatives displayed good inhibition against the growth of the human colon cancer HCT116 cell line, with potencies lower than but in the same order of magnitude as camptothecin (CPT). These two luotonin analogues also sho  ...[more]

Similar Datasets

Unknown Design and synthesis of DNA-intercalative naphthalimide-benzothiazole/cinnamide derivatives: cytotoxicity evaluation and topoisomerase-IIα inhibition.
| S-EPMC6350626 | biostudies-literature
Unknown Design, synthesis and cytotoxicity of bengamide analogues and their epimers.
| S-EPMC6072509 | biostudies-literature
Unknown Design, Synthesis, and Study of Lactam and Ring-Expanded Analogues of Teixobactin.
| S-EPMC7814697 | biostudies-literature
Unknown Synthesis and photobiological applications of naphthalimide-benzothiazole conjugates: cytotoxicity and topoisomerase IIα inhibition.
| S-EPMC8694140 | biostudies-literature
Unknown Design, Synthesis, and Cytotoxicity Evaluation of Novel Griseofulvin Analogues with Improved Water Solubility.
| S-EPMC5738580 | biostudies-literature
Unknown Design, Synthesis and Cytotoxicity of Thiazole-Based Stilbene Analogs as Novel DNA Topoisomerase IB Inhibitors.
| S-EPMC8838847 | biostudies-literature
Unknown Design, Synthesis and Antitumor Activity of Novel link-bridge and B-Ring Modified Combretastatin A-4 (CA-4) Analogues as Potent Antitubulin Agents.
| S-EPMC4853715 | biostudies-literature
Unknown Facile Synthesis of Some Coumarin Derivatives and Their Cytotoxicity through VEGFR2 and Topoisomerase II Inhibition.
| S-EPMC9737644 | biostudies-literature
Unknown Design and synthesis of diazine-based panobinostat analogues for HDAC8 inhibition.
| S-EPMC7155894 | biostudies-literature
Unknown <i>cis</i>-Diastereoselective synthesis of chroman-fused tetralins as B-ring-modified analogues of brazilin.
| S-EPMC5238543 | biostudies-literature