Novel 1,3,4-heterodiazole analogues: Synthesis and in- vitro antitumor activity
The synthesis of some new heterodiazole and their annulated imidazo[2,1- b]1,3,4-oxa/thiadiazolone 6a– d, 7a– d; 1,3,4-oxa or thiadiazole[3,2- a]pyrimidine diamine 8a– d and 1,3,4-oxa or thiadiazole-3-piperidino-1-propamide 11a, b derivatives have been described. The obtained compounds were evaluate...
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Veröffentlicht in: | European journal of medicinal chemistry 2012, Vol.47 (1), p.445-451 |
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Hauptverfasser: | , , |
Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | The synthesis of some new heterodiazole and their annulated imidazo[2,1-
b]1,3,4-oxa/thiadiazolone
6a–
d,
7a–
d; 1,3,4-oxa or thiadiazole[3,2-
a]pyrimidine diamine
8a–
d and 1,3,4-oxa or thiadiazole-3-piperidino-1-propamide
11a,
b derivatives have been described. The obtained compounds were evaluated for their
in-
vitro antitumor activity. A single dose (10 μM) of the test compounds were used in the full National Cancer Institute (NCI) 60 cell lines panel assay. Compounds
6c and
6d displayed appreciable anticancer activity against leukemia, non-small cell lung, CNS and showed moderate activity against colon, melanoma, and breast cancer cells lines. Compound
6c possessed remarkable broad-spectrum antitumor activity which almost 4 fold more active than the known drug 5-FU with GI
50, TGI, and LC
50 values of 6.0, 17.4, and 55.1 μM, respectively.
The manuscript deals with the synthesis of 1,3,4-oxa/thiadiazole and their annelated imidazo[2,1-
b]1,3,4-oxa/thiadiazolone derivatives. The obtained compounds were evaluated for their
in-
vitro antitumor activity.
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► Series of 1,3,4-oxa or thiadiazole and their cyclized derivatives were prepared. ► The
in-
vitro evaluations were used in the NCI 60 cell lines panel assay. ► Compounds
6c,
d showed appreciable activity against leukemia, non-small cell lung and CNS. ► Compound
6c proved to be the most active member of this study. |
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ISSN: | 0223-5234 1768-3254 |
DOI: | 10.1016/j.ejmech.2011.11.013 |