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Design, synthesis and biological evaluation of Novel Curcumin Analogs with anticipated anticancer activity

Fawzy, Iten M. (author)
Future Univ, Fac Pharmaceut Sci & Pharmaceut Ind, Pharmaceut Chem Dept, Cairo 12311, Egypt.
Youssef, Khairia M. (author)
Future Univ, Fac Pharmaceut Sci & Pharmaceut Ind, Pharmaceut Chem Dept, Cairo 12311, Egypt.
Ismail, Nasser S. M. (author)
Ain Shams Univ, Fac Pharm, Pharmaceut Chem Dept, Cairo, Egypt.
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Gullbo, Joachim (author)
Uppsala universitet,Cancerfarmakologi och beräkningsmedicin
Abouzid, Khaled A. M. (author)
Ain Shams Univ, Fac Pharm, Pharmaceut Chem Dept, Cairo, Egypt.
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Future Univ, Fac Pharmaceut Sci & Pharmaceut Ind, Pharmaceut Chem Dept, Cairo 12311, Egypt Ain Shams Univ, Fac Pharm, Pharmaceut Chem Dept, Cairo, Egypt. (creator_code:org_t)
ELSEVIER SCIENCE BV, 2015
2015
English.
In: FUTURE JOURNAL OF PHARMACEUTICAL SCIENCES. - : ELSEVIER SCIENCE BV. - 2314-7245. ; 1:1, s. 22-31
  • Journal article (peer-reviewed)
Abstract Subject headings
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  • Context: Extensive research conducted within past years revealed that curcumin is a highly pleiotropic molecule that interacts with a diverse range of molecular targets and hence it possess anti-proliferative activities against tumor cells.The great similarities between curcumin analogs and chalcones inspired their testing against tubulin enzyme activity as recent research revealed that chalcones possess cytotoxic activity associated with tubulin inhibition and interference with microtubule formation, which is essential in mitosis and cell replication. Objective: Novel Curcumin analogs were designed, synthesized and tested for their antitumor activities. Also in silico and in vitro studies has been performed to predict the binding affinity of the target compounds and to test their ability to inhibit tubulin assembly and act as microtubule destabilizing agents. Methods: Six novel curcumin analogs were designed & synthesized with 3,5-dibenzylidenepiperidin-4-one core moiety. Results: Compounds showed interaction energy comparable to or within the range of podophyllotoxin itself when docked into the colchicine binding site of tubulin using the podophyllotoxin-tubulin complex (PDB 1SA1). Conclusion: Compounds showed moderate anticancer activity and moderate ability to destabilize microtubules and thus inhibiting tubulin polymerization, as a result; these compounds could be used for further future development to obtain more potent analogs. (C) 2015 Future University. Production and hosting by Elsevier B.V.

Subject headings

MEDICIN OCH HÄLSOVETENSKAP  -- Medicinska och farmaceutiska grundvetenskaper -- Farmakologi och toxikologi (hsv//swe)
MEDICAL AND HEALTH SCIENCES  -- Basic Medicine -- Pharmacology and Toxicology (hsv//eng)
MEDICIN OCH HÄLSOVETENSKAP  -- Medicinska och farmaceutiska grundvetenskaper -- Cell- och molekylärbiologi (hsv//swe)
MEDICAL AND HEALTH SCIENCES  -- Basic Medicine -- Cell and Molecular Biology (hsv//eng)

Keyword

Curcumin analogs
In silico molecular docking
Anti proliferative activity
Tubulin polymerization

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ref (subject category)
art (subject category)

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