Bookmark and Share
BioAssay: AID 442505

Inhibition of PTK

A series of sulfapyridine-polyhydroxyalkylidene (or arylidene)-imino derivatives (Schiff's bases) 2a-c and 4a-e were prepared by condensation of 4-amino-N-pyridin-2-ylbenzenesulfonamide (1) with different monosaccharides or with aromatic aldehydes. Treatment of 2a-c with thioglycolic acid led to the formation of the C-nucleosides (3a-c), while treatment of 4a-e with thioglycolic and/or more ..
_
   
 Tested Compounds
 Tested Compounds
All(23)
 
 
Active(22)
 
 
Unspecified(1)
 
 
 Tested Substances
 Tested Substances
All(23)
 
 
Active(22)
 
 
Unspecified(1)
 
 
 Related BioAssays
 Related BioAssays
AID: 442505
Data Source: ChEMBL (593683)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-07-08
Modify Date: 2014-05-25

Data Table ( Complete ):           View Active Data    View All Data
BioActive Compounds: 22
Description:
Title: Synthesis, antitumor activity and molecular docking study of novel sulfonamide-Schiff's bases, thiazolidinones, benzothiazinones and their C-nucleoside derivatives.

Abstract: A series of sulfapyridine-polyhydroxyalkylidene (or arylidene)-imino derivatives (Schiff's bases) 2a-c and 4a-e were prepared by condensation of 4-amino-N-pyridin-2-ylbenzenesulfonamide (1) with different monosaccharides or with aromatic aldehydes. Treatment of 2a-c with thioglycolic acid led to the formation of the C-nucleosides (3a-c), while treatment of 4a-e with thioglycolic and/or thiosalicylic acids afforded the corresponding 2-arylthiazolidin-4-one or 2-arylbenzothiazin-4-one derivatives 5a-e and/or 6a-e, respectively. Some representative examples of the newly prepared compounds showed considerable cytotoxic effect against breast carcinoma cell line MCF7 and cervix carcinoma cell line HELA in comparison with 5-flurouracil and doxorubicin. AutoDock molecular docking into PTK has been done for lead optimization of the compounds in study as potential PTK inhibitors.
(PMID: 19932530)
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 - additional comments and annotations
From ChEMBL:
Assay Type: Binding
Assay Data Source: Scientific Literature
Result Definitions
Show more
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Ki*Ki PubChem standard valueFloatμM
2Ki activity commentKi activity commentString
3Ki standard flagKi standard flagInteger
4Ki qualifierKi qualifierString
5Ki published valueKi published valueFloat10'-14M
6Ki standard valueKi standard valueFloatnM
7Ki data validityKi data validityString
8Ki activity commentKi activity commentString
9Ki standard flagKi standard flagInteger
10Ki qualifierKi qualifierString
11Ki published valueKi published valueFloat10'-4M
12Ki standard valueKi standard valueFloatnM
13Ki data validityKi data validityString
14Ki activity commentKi activity commentString
15Ki standard flagKi standard flagInteger
16Ki qualifierKi qualifierString
17Ki published valueKi published valueFloat10'-5M
18Ki standard valueKi standard valueFloatnM
19Ki data validityKi data validityString
20Ki activity commentKi activity commentString
21Ki standard flagKi standard flagInteger
22Ki qualifierKi qualifierString
23Ki published valueKi published valueFloat10'-6M
24Ki standard valueKi standard valueFloatnM
25Ki data validityKi data validityString
26Ki activity commentKi activity commentString
27Ki standard flagKi standard flagInteger
28Ki qualifierKi qualifierString
29Ki published valueKi published valueFloat10'-7M
30Ki standard valueKi standard valueFloatnM
31Ki data validityKi data validityString
32Ki activity commentKi activity commentString
33Ki standard flagKi standard flagInteger
34Ki qualifierKi qualifierString
35Ki published valueKi published valueFloat10'-8M
36Ki standard valueKi standard valueFloatnM
37Ki data validityKi data validityString

* Activity Concentration.

Data Table (Concise)
Data Table ( Complete ):     View Active Data    View All Data
PageFrom: