title: Novel all trans-retinoic Acid derivatives: cytotoxicity, inhibition of cell cycle progression and induction of apoptosis in human cancer cell lines.
abstract: Owing to the pharmacological potential of ATRA (all trans-retinoic acid), a series of retinamides and a 1-(retinoyl)-1,3-dicyclohexylurea compound were prepared by reacting ATRA with long chain alkyl or alkenyl fatty amines by using a 4-demethylaminopyridine (DMAP)-catalyzed N,N¢-dicyclohexylcarbodiimide (DCC) coupling. The successful synthesis of the target compounds was demonstrated using a range of spectroscopic techniques. The cytotoxicity of the compounds was measured along with their ability to induce cell cycle arrest and apoptosis in human cancer cell lines MCF-7 (breast cancer) and HepG2 (liver cancer) and normal human cell line HEK293 (embryonic kidney). The results of cytotoxicity and flow cytometry data showed that the compounds had a moderate to strong effect against MCF-7 and HepG2 cells and were less toxic to HEK293 cells. N-oleyl-retinamide was found to be the most potent anticancer agent and was more effective against MCF-7 cells than HepG2 cells.
authors.affiliation: Department of Pharmacognosy, College of Pharmacy, King Saud University, Riyadh 11495, Saudi Arabia. ebtesam.saad@yahoo.com.
authors.forename: Ebtesam Saad
authors.initials: ES
authors.lastname: Al-Sheddi
authors.affiliation: Department of Pharmacognosy, College of Pharmacy, King Saud University, Riyadh 11495, Saudi Arabia. maioqail@hotmail.com.
authors.forename: Mai Mohammad
authors.initials: MM
authors.lastname: Al-Oqail
authors.affiliation: Zoology Department, College of Science, King Saud University, Riyadh 11451, Saudi Arabia. quaiser.saquib0@gmail.com.|Al-Jeraisy Chair for DNA Research, College of Science, King Saud University, Riyadh 11451, Saudi Arabia. quaiser.saquib0@gmail.com.
authors.forename: Quaiser
authors.initials: Q
authors.lastname: Saquib
authors.affiliation: Zoology Department, College of Science, King Saud University, Riyadh 11451, Saudi Arabia. maqsoodahmads@gmail.com.|Al-Jeraisy Chair for DNA Research, College of Science, King Saud University, Riyadh 11451, Saudi Arabia. maqsoodahmads@gmail.com.
authors.forename: Maqsood Ahmed
authors.initials: MA
authors.lastname: Siddiqui
authors.affiliation: Zoology Department, College of Science, King Saud University, Riyadh 11451, Saudi Arabia. musarratj1@yahoo.co.in.|Al-Jeraisy Chair for DNA Research, College of Science, King Saud University, Riyadh 11451, Saudi Arabia. musarratj1@yahoo.co.in.
authors.forename: Javed
authors.initials: J
authors.lastname: Musarrat
authors.affiliation: Zoology Department, College of Science, King Saud University, Riyadh 11451, Saudi Arabia. kedhairy@yahoo.com.
authors.forename: Abdulaziz Ali
authors.initials: AA
authors.lastname: Al-Khedhairy
authors.affiliation: Department of Pharmacognosy, College of Pharmacy, King Saud University, Riyadh 11495, Saudi Arabia. nidachem@gmail.com.
authors.forename: Nida Nayyar
authors.initials: NN
authors.lastname: Farshori
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects*; D001943:Breast Neoplasms / Q000188:drug therapy; D059447:Cell Cycle Checkpoints / Q000187:drug effects*; D002460:Cell Line; D045744:Cell Line, Tumor; D005260:Female; D057809:HEK293 Cells; D056945:Hep G2 Cells; D006801:Humans; D008113:Liver Neoplasms; D061986:MCF-7 Cells; D014212:Tretinoin / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology*; D014508:Urea / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D014212:Tretinoin; D014508:Urea; C054441:retinamide; C000948:1,3-dicyclohexylurea