Open AccessThe Synthesis and Preliminary Anticancer Evaluation of 6-Mercaptopurine -Methotrexate Conjugate as Possible Mutual Prodrug
Author(s) -
Asmaa Safwan Al-darraji,
Mohamed H.Mohamed
Publication year - 2019
Publication title -
al-maǧallaẗ al-’irāqiyyaẗ li-l-’ulūm al-ṣaydalāniyyaẗ/iraqi journal of pharmaceutical sciences
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.122
H-Index - 1
eISSN - 2521-3512
pISSN - 1683-3597
DOI - 10.31351/vol28iss1pp114-124
Subject(s) - prodrug , conjugate , chemistry , combinatorial chemistry , lead compound , cancer cell lines , stereochemistry , pharmacology , cancer cell , biochemistry , cancer , medicine , mathematical analysis , mathematics , in vitro
Small molecules drug conjugate mutual prodrug design (SMDC) composed of folate &lethal agent conjugate , rigidly bonded via hydrophilic bridge& self immolative disulfide bond ; represent new interesting approaches for cancer treatment , the component of SMDC intended to be as possible suit targeted folate receptor , along with greater conservation of component until reaching targeting tumor tissue . The designing & synthesis of compound VI & IIX derived from 6-MP & MTX conjugate altogether as mutual prodrug were processed forward successfully by multiple steps procedure , and by TLC spectrophotometry preliminary analysis assess in detection of products & their intermediate , along with their purity . The structure of two final compounds & their intermediate were proclaimed by melting point measurement , infrared spectrometry & HNMR analysis given results greatly correspond with theoretical proposed chemical structure of synthesized compounds . Furthermore anticancer evaluation on cell line level had been done for two final compound against MCF-7& SKO-3 types of cancer cell & the result were confirmed which show greater cytotoxic tumor activity of two final compound ,while compound IIX possess optimal activity proportional with increase number of 6-MP residue .