Multicomponent access to novel proline cyclized cysteine tethered monastrol conjugates as potential anticancer agents
Joint Authors
Kamal, Ahmad
Jamal, Qazi Muhd. Sajid
Malik, M. Shahir
Sadiki, Zaki S.
Baji, Shaik
Azizah, Shaik
al-Thaqfi, Ismail I.
Sayyid, Riyad A.
Ahmad, Salih A. M.
Source
Journal of Saudi Chemical Society
Issue
Vol. 23, Issue 4 (31 May. 2019), pp.503-513, 11 p.
Publisher
Publication Date
2019-05-31
Country of Publication
Saudi Arabia
No. of Pages
11
Main Subjects
Topics
Abstract EN
The versatility of multicomponent Biginelli’s reaction is exploited in the development of proline and cyclized cysteine tethered conjugates of monastrol, a kinesin Eg5 inhibitor.
Ten new conjugates are synthesized focusing on structural replacement of the ester moiety (C-5 position) of the monastrol backbone with amino acid based amide moieties.
On cytotoxic evaluation, conjugate 24 has shown promising in vitro cytotoxic activity against leukemia.
Molecular docking studies revealed that the conjugates 19 and 24 exhibit better interaction at kinesin Eg5 receptor compared to monastrol.
Moreover, computational calculations and predictions of important molecular properties suggest that these new amino acid based conjugates could be further improved to provide potential anticancer agents
American Psychological Association (APA)
Malik, M. Shahir& Sadiki, Zaki S.& Sayyid, Riyad A.& Ahmad, Salih A. M.& Jamal, Qazi Muhd. Sajid& Kamal, Ahmad…[et al.]. 2019. Multicomponent access to novel proline cyclized cysteine tethered monastrol conjugates as potential anticancer agents. Journal of Saudi Chemical Society،Vol. 23, no. 4, pp.503-513.
https://search.emarefa.net/detail/BIM-894824
Modern Language Association (MLA)
Sayyid, Riyad A.…[et al.]. Multicomponent access to novel proline cyclized cysteine tethered monastrol conjugates as potential anticancer agents. Journal of Saudi Chemical Society Vol. 23, no. 4 (May. 2019), pp.503-513.
https://search.emarefa.net/detail/BIM-894824
American Medical Association (AMA)
Malik, M. Shahir& Sadiki, Zaki S.& Sayyid, Riyad A.& Ahmad, Salih A. M.& Jamal, Qazi Muhd. Sajid& Kamal, Ahmad…[et al.]. Multicomponent access to novel proline cyclized cysteine tethered monastrol conjugates as potential anticancer agents. Journal of Saudi Chemical Society. 2019. Vol. 23, no. 4, pp.503-513.
https://search.emarefa.net/detail/BIM-894824
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references : p. 513
Record ID
BIM-894824