Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
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Enzyme
Compound
Query: UMLS:C0699790 (
colon cancer
)
28,837
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
The African tree
Combretum caffrum
(Combretacae) has been found to contain a powerful inhibitor of tubulin polymerization (IC50 2-3 microM), the growth of murine lymphocytic leukemia (L 1210 and P 388 with ED50 approximately 0.003 microM and human
colon cancer
cell lines [(e.g. LoVo (ED50 = 0.005 microgram/ml), HT 29 (ED50 0.02 microgram/ml, Colo 205 (ED50 = 0.07 microgram/ml), DLD-1 (ED50 = 0.005 microgram/ml) and HCT-15 (ED50 = 0.0009 microgram/ml] designated combretastatin A-4 (1c). The structure assigned by spectral techniques was confirmed by synthesis.
...
PMID:Isolation and structure of the strong cell growth and tubulin inhibitor combretastatin A-4. 292 Aug 9
Several synthetic combretastatin A4 (
CA-4
) derivatives were recently prepared to increase the drug efficacy and stability of the natural product isolated from the South African tree
Combretum caffrum
. A group of ten 3-amino-2-azetidinone derivatives, as combretastatin A4 analogues, was selected through docking experiments, synthesized and tested for their anti-proliferative activity against the
colon cancer
SW48 cell line. These molecules, through the formation of amide bonds in position 3, allow the synthesis of various derivatives that can modulate the activity with great resistance to hydrolytic conditions. The cyclization to obtain the 3-aminoazetidinone ring is highly diastereoselective and provides a
trans
biologically active isomer under mild reaction conditions with better yields than the 3-hydroxy-2-azetidinone synthesis. All compounds showed IC
50
values ranging between 14.0 and 564.2 nM, and the most active compound showed inhibitory activity against tubulin polymerization
in vitro
, being a potential therapeutic agent against
colon cancer
.
...
PMID:Synthesis and biological evaluation of new 3-amino-2-azetidinone derivatives as anti-colorectal cancer agents. 3010 73
