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19th April 2012 @ 04:51

Data obtained for compounds synthesised by Soumya Bhattacharyya and Sanjay Batra.

Conclusions: 1) 3-fluoro "near neighbour" derivative is much less active than closely related compounds described here. 2) The IC50 for PMY 10-6 broadly matches the results obtained by other labs, meaning this is a good control to use in conjunction with chloroquine.

Data for (3-fluorophenyl) pyrrole derivative SBBH-1-9 (or isomer) Synthesis of (3E)-3-((1-(3-fluorophenyl)-2,5-dimethyl-1H-pyrrol-3-yl)methylene)-1-phenyl-5-(phenylimino)pyrrolidin-2-one or it’s isomer (SBBH-1-9)

(Original data posted to G+ (with wrong name) - screenshot attached)

3D7:

Sample Code, IC50 (microM), CC50 (microM), SI SBBH-1-9: 3.2, 92.4, 28.87 Chloroquine: 0.0063, 125.85, 19976.2

K1 strain:

Sample Code, IC50 (microM,) CC50 (microM), SI SBBH-1-9: >5.0, 92.4, 18.48 Chloroquine: 0.235, 125.85, 535.53

Original 3-F data

Control compounds sent from Sydney was PMY 10-6 (TCMDC-123812) Synthesis of TCMDC-123812 via acid chloride (PMY 10-6), which was evaluated (13/04/2012) vs.chloroquine. Data attached

Controls

and results pasted here:

For 3D7: PMY 10-6 IC50 0.581 microM, CC50 (cytotoxicity) nd, SI (selectivity index) - CQ IC50 0.0083 microM, CC50 125.85, SI 15162.7

For K1: PMY 10-6 IC50 0.641, CC50 nd, SI - CQ IC50 0.252, CC50 125.85, SI 499

Method used for cytotoxicity assay:

cytotox assay SOP

In more recent correspondence in late 2014, assay protocol was updated by Sanjay Batra:

Text S Assay Protocol Batra New.docx
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Attached Files
Controls
Original 3-F data
cytotox assay SOP
Text S Assay Protocol Batra New.docx