TY  - BOOK
AU  - Waleed Nabeel Saeed Aldarkazali
AU  - Nadia Yaha Megally Abdo , 
AU  - Naglaa Yousef Samy , 
AU  - Rafat Melad Mohareb , 
TI  - New approaches for the synthesis and cytotoxicity of novel heterocyclic compounds derived from Ý-dicarbonyl and cyanomethylene reagents / 
PY  - 2018///
CY  - Cairo : 
PB  - Waleed Nabeel Saeed Aldarkazali , 
KW  - Cyclohexan-1,3-dione
KW  - Thiazole
KW  - Thiophene
N1  - Thesis (M.Sc.) - Cairo University - Faculty of Science - Department of Organic Chemistry; Issued also as CD
N2  - The reaction of cyclohexan-1,3-dione (1) with benzaldhyde, 4-chlorobenzaldhyde and 4-methoxy benzaldhyde (2a-c) in ethanol in the presence of catalytic amount of piperidine  afforded 2-Arylidencyclohexan-1,3-dione 3a-c. The latter compounds reacted with elemental sulfer and either of malonanitrile (4a) or ethyl cyanoacetate (4b) in 1,4-dioxan in the presence of triethylamine to give tetrahydrobenzo[b]thiophen-5-one derivatives 5a-f. Compounds 5a, b were used for the synthesis of thiophene, thiazole and isoxazale derivatives through their reactions with different chemical reagents. The analytical and spectral data of newly synthesized compounds were consistent with their respective structures. The anti-proliferative activities of the newly synthesized compounds were evaluated against the six cancer cell lines  A549, HT-29, MKN-45, U87MG, SMMC-7721 and H460. The most potent compounds  toward the cancer cell lines 3a, 3c, 5d, 7c, 11c, 16a, 16c, 17a, 19f, 20a, 21c, 23a and 23c, were further investigated towards the five tyrosine kinases c-kit, FIT-3, VEGFR-2, EGFR and  PDGFR. Compounds 3c, 5d, 16c, 17a, 19f and 21c were selected for testing of their inhibition  for the Pim-1 kinase due to their anti-proliferation activities against the cancer cell lines and  their high activities against the tyrosine kinases
UR  - http://172.23.153.220/th.pdf
ER  -