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

المؤلفون المشاركون

Suresh Kumar, Raju
Almansour, Abdulrahman I.
Arumugam, Natarajan
Bianchini, Giulia
Menéndez, J. Carlos
Mohammad, Faruq
Dupadahalli, Kotresha
Altaf, Mohammad

المصدر

BioMed Research International

العدد

المجلد 2019، العدد 2019 (31 ديسمبر/كانون الأول 2019)، ص ص. 1-12، 12ص.

الناشر

Hindawi Publishing Corporation

تاريخ النشر

2019-11-13

دولة النشر

مصر

عدد الصفحات

12

التخصصات الرئيسية

الطب البشري

الملخص EN

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.

نمط استشهاد جمعية علماء النفس الأمريكية (APA)

Almansour, Abdulrahman I.& Suresh Kumar, Raju& Arumugam, Natarajan& Bianchini, Giulia& Menéndez, J. Carlos& Mohammad, Faruq…[et al.]. 2019. D-Ring-Modified Analogues of Luotonin A with Reduced Planarity: Design, Synthesis, and Evaluation of Their Topoisomerase Inhibition-Associated Cytotoxicity. BioMed Research International،Vol. 2019, no. 2019, pp.1-12.
https://search.emarefa.net/detail/BIM-1123889

نمط استشهاد الجمعية الأمريكية للغات الحديثة (MLA)

Almansour, Abdulrahman I.…[et al.]. D-Ring-Modified Analogues of Luotonin A with Reduced Planarity: Design, Synthesis, and Evaluation of Their Topoisomerase Inhibition-Associated Cytotoxicity. BioMed Research International No. 2019 (2019), pp.1-12.
https://search.emarefa.net/detail/BIM-1123889

نمط استشهاد الجمعية الطبية الأمريكية (AMA)

Almansour, Abdulrahman I.& Suresh Kumar, Raju& Arumugam, Natarajan& Bianchini, Giulia& Menéndez, J. Carlos& Mohammad, Faruq…[et al.]. D-Ring-Modified Analogues of Luotonin A with Reduced Planarity: Design, Synthesis, and Evaluation of Their Topoisomerase Inhibition-Associated Cytotoxicity. BioMed Research International. 2019. Vol. 2019, no. 2019, pp.1-12.
https://search.emarefa.net/detail/BIM-1123889

نوع البيانات

مقالات

لغة النص

الإنجليزية

الملاحظات

Includes bibliographical references

رقم السجل

BIM-1123889