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Open AccessArticle

Potent Anti-Ovarian Cancer with Inhibitor Activities on Both Topoisomerase II and V600EBRAF of Synthesized Substituted Estrone Candidates

1
Chemistry Department, Faculty of Sciences, University of Sharjah, Sharjah 27272, UAE
2
Drug Exploration & Development Chair (DEDC), Pharmaceutical Chemistry Department, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia
3
Applied Organic Chemistry Department, National Research Center, Cairo 12622, Egypt
4
Respiratory Therapy Department, College of Medical Rehabilitation Sciences, Taibah University, Madinah Munawara 22624, Saudi Arabia
5
Zoology Department, Bioproducts Research Chair, College of Science, King Saud University, Riyadh 11451, Saudi Arabia
6
Chemistry of Natural and Microbial Products Department, National Research Centre, Cairo 12622, Egypt
7
Atos Pharma, Elkatyba Land, Belbis 44621, El Sharkya, Egypt
*
Author to whom correspondence should be addressed.
Molecules 2019, 24(11), 2054; https://doi.org/10.3390/molecules24112054
Received: 25 April 2019 / Revised: 23 May 2019 / Accepted: 28 May 2019 / Published: 29 May 2019
(This article belongs to the Special Issue Anticancer Agents: Design, Synthesis and Evaluation)
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Abstract

A series of 16-(α-alkoxyalkane)-17-hydrazino-estra-1(10),2,4-trien[17,16-c]-3-ol (3al) and estra-1(10),2,4-trien-[17,16-c]pyrazoline-3-ol derivatives (4ad) were synthesized from corresponding arylidines 2a,b which was prepared from estrone 1 as starting material. Condensation of 1 with aldehydes gave the corresponding arylidine derivatives 2a,b which were treated with hydrazine derivatives in alcohols to give the corresponding derivatives 3al, respectively. Additionally, treatment of 2a,b with methyl- or phenylhydrazine in ethanolic potassium hydroxide afforded the corresponding N-substituted pyrazoline derivatives 4ad, respectively. All these derivatives showed potent anti-ovarian cancer both in vitro and in vivo. The mechanism of anti-ovarian cancer was suggested to process via topoisomerase II and V600EBRAF inhibition. View Full-Text
Keywords: estrone derivatives; hydrazine; N-substituted pyrazoline; anti-ovarian cancer; topoisomerase II inhibitor; kinase inhibitor estrone derivatives; hydrazine; N-substituted pyrazoline; anti-ovarian cancer; topoisomerase II inhibitor; kinase inhibitor
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El-Naggar, M.; E. Amr, A. .-G.; Fayed, A.A.; A. Elsayed, E.; A. Al-Omar, M.; Abdalla, M.M. Potent Anti-Ovarian Cancer with Inhibitor Activities on Both Topoisomerase II and V600EBRAF of Synthesized Substituted Estrone Candidates. Molecules 2019, 24, 2054.

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