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03-10-2006, 10:54 AM

research from the pesticide chemistry research department in Cairo, Egypt! (unfortunately he is not using a her2 + cell line in his studies...yet)

Bioorg Med Chem. 2006 Mar 6; [Epub ahead of print] Links

Novel synthesis of nicotinamide derivatives of cytotoxic properties.

Girgis AS, Hosni HM, Barsoum FF.

Pesticide Chemistry Department, National Research Centre, Dokki, 12622 Cairo, Egypt.

A variety of 2-substituted-4,6-diaryl-3-pyridinecarboxamides 5 were synthesized through aromatic nucleophilic substitution reaction of secondary amines with 2-bromo analogues 4. The latter were obtained via bromination of 2-cyano-3,5-diaryl-5-oxo-N-substituted pentamides 3 in glacial acetic acid. Moreover, pentamide derivatives 3 were prepared through base-catalyzed Michael addition of cyanacetanilides 2 with 1,3-diaryl-2-propen-1-ones 1. Otherwise, reaction of 2-bromo-3-pyridinecarboxamides 4 with primary aromatic amines in refluxing pyridine afforded the corresponding 2-(arylamino)-3-pyridinecarboxamides 6 besides the unexpected 2-unsubstituted amino analogues 7. Antitumor properties of the synthesized pyridinecarboxamides utilizing 59 different human tumor cell lines, representing leukemia, melanoma, and cancers of the lung, colon, brain, ovary, breast, prostate as well as kidney, were screened. Many of the tested compounds show considerable in vitro antitumor properties especially 5c and 7a, which reveal moderate activities against most of the used human tumor cell lines. It has also been achieved that, all the tested nicotinamide derivatives reveal promising antitumor properties against MDA-MB-231/ATCC (breast cancer).

PMID: 16524735 [PubMed - as supplied by publisher]

03-10-2006, 10:54 AM	#1
Lani Guest Posts: n/a	for Rhonda H--maybe something good can come from something bad... research from the pesticide chemistry research department in Cairo, Egypt! (unfortunately he is not using a her2 + cell line in his studies...yet) Bioorg Med Chem. 2006 Mar 6; [Epub ahead of print] Links Novel synthesis of nicotinamide derivatives of cytotoxic properties. Girgis AS, Hosni HM, Barsoum FF. Pesticide Chemistry Department, National Research Centre, Dokki, 12622 Cairo, Egypt. A variety of 2-substituted-4,6-diaryl-3-pyridinecarboxamides 5 were synthesized through aromatic nucleophilic substitution reaction of secondary amines with 2-bromo analogues 4. The latter were obtained via bromination of 2-cyano-3,5-diaryl-5-oxo-N-substituted pentamides 3 in glacial acetic acid. Moreover, pentamide derivatives 3 were prepared through base-catalyzed Michael addition of cyanacetanilides 2 with 1,3-diaryl-2-propen-1-ones 1. Otherwise, reaction of 2-bromo-3-pyridinecarboxamides 4 with primary aromatic amines in refluxing pyridine afforded the corresponding 2-(arylamino)-3-pyridinecarboxamides 6 besides the unexpected 2-unsubstituted amino analogues 7. Antitumor properties of the synthesized pyridinecarboxamides utilizing 59 different human tumor cell lines, representing leukemia, melanoma, and cancers of the lung, colon, brain, ovary, breast, prostate as well as kidney, were screened. Many of the tested compounds show considerable in vitro antitumor properties especially 5c and 7a, which reveal moderate activities against most of the used human tumor cell lines. It has also been achieved that, all the tested nicotinamide derivatives reveal promising antitumor properties against MDA-MB-231/ATCC (breast cancer). PMID: 16524735 [PubMed - as supplied by publisher]