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BioAssay: AID 361969

Antiproliferative activity against estrogen receptor deficient human MDA468 cells after 72 hrs by MTT assay

New fluorinated 2-aryl-benzothiazoles, -benzoxazoles, and -chromen-4-ones have been synthesized and their activity against MCF-7 and MDA 468 breast cancer cell lines compared with the potent antitumor benzothiazole 5. Analogues such as 9a, b and 12a, d yielded submicromolar GI50 values in both cell lines; however, none of the new compounds approached 5 in terms of antitumor potency. For 5, binding to the aryl hydrocarbon receptor appeared to be necessary but not sufficient for growth inhibition. ..more
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 Tested Compounds
 Tested Compounds
All(32)
 
 
Active(28)
 
 
Unspecified(4)
 
 
 Tested Substances
 Tested Substances
All(32)
 
 
Active(28)
 
 
Unspecified(4)
 
 
 Related BioAssays
 Related BioAssays
AID: 361969
Data Source: ChEMBL (509998)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-26
Modify Date: 2013-07-20

Data Table ( Complete ):           Active    All
BioActive Compounds: 28
Description:
Title: Synthesis and biological properties of benzothiazole, benzoxazole, and chromen-4-one analogues of the potent antitumor agent 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole (PMX 610, NSC 721648).

Abstract: New fluorinated 2-aryl-benzothiazoles, -benzoxazoles, and -chromen-4-ones have been synthesized and their activity against MCF-7 and MDA 468 breast cancer cell lines compared with the potent antitumor benzothiazole 5. Analogues such as 9a, b and 12a, d yielded submicromolar GI50 values in both cell lines; however, none of the new compounds approached 5 in terms of antitumor potency. For 5, binding to the aryl hydrocarbon receptor appeared to be necessary but not sufficient for growth inhibition.
(PMID: 18666770)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Putative Target:

ChEMBL Target ID: 22226
Target Type: UNCHECKED
Pref Name: Unchecked
Confidence: Default value - Target unknown or has yet to be assigned
Relationship Type: Default value - Target has yet to be curated
Categorized Comment
ChEMBL Assay Type: Functional

ChEMBL Assay Data Source: Scientific Literature

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1GI50*GI50 PubChem standard valueFloatμM
2GI50 activity commentGI50 activity commentString
3GI50 standard flagGI50 standard flagInteger
4GI50 qualifierGI50 qualifierString
5GI50 published valueGI50 published valueFloatμM
6GI50 standard valueGI50 standard valueFloatnM
7GI50 data validityGI50 data validityString

* Activity Concentration.

Data Table (Concise)
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