No abstract

A series of aroyl derivatives of 4-(2-chloroethyl)semicarbazide were designed and synthesized to explore their antiproliferative activity against human brain carcinoma (U251) and human liver carcinoma (Hepg2) cell lines. The synthesized compounds were characterized by elemental analyses and spectroscopic data. It was established that compounds in which semicarbazide fragments are substituted with a (2-indolyl)carbonyl moiety showed a higher cytotoxic activity than the corresponding benzoyl derivatives. 1-[(5-Benzyloxy-1H-indol-2-yl)carbonyl]-4-(2-chloroethyl)semicarbazide (24) showed the highest cytotoxic activity against Hepg2 (IC 50 = 21 mg/ml), while 4-(2-chloroethyl)-1-[(5-methoxy-1H-indol-2-yl)carbonyl]semicarbazide (23) was the most active compound against U251 (IC 50 = 8 mg/ml).

No abstract

No abstract

Synthesis of Hexahydro-1H-pyrido[3,2-c]azepines as Hypotensive Agents of Expected Calcium-Channel Blocking Activity. -A series of novel pyridoazepine derivatives (13 examples), structurally related to nifedipine, is synthesized via Michael reaction of enaminones (I) to acrylonitrile derivatives (II) followed by ring enlargement of the obtained hexahydroquinolines (III) under Schmidt reaction conditions. Derivatives (V) exhibit the highest hypotensive activity and negative inotropic as well as chronotropic activity. -(EL-SADEK, M. E.; ABOUKULL, M.; EL-SABBAGH*, O. I.; SHALLAL, H. M.; Monatsh. Chem. 138 (2007) 3, 219-225; Dep. Med. Chem., Fac. Pharm., Zagazig Univ., Zagazig, Egypt; Eng.) -R. Langenstrassen 25-165