Development and investigation of thiazolidinedione and pyrazoline compounds as antiangiogenic weapons targeting VEGFR-2
Background: Angiogenesis deregulation is often linked to cancer and is thus an essential target. Materials & methods: Twenty-nine compounds were developed as VEGFR-2 inhibitors. Compounds were evaluated to determine their antiangiogenic activity. Results: B1, PB11 and PB16 showed HUVEC's IC50 scores in the submicromolar range. B1, B2 and PB16 reduced cellular migration and capillary tube formation of HUVECs. VEGFR-2 inhibitory activity was found in the nanomolar range: 200 nM of B1, 500 nM of B2 and 600 nM of PB16. B1 and PB16 suppressed the formation of new capillaries on growing CAMs. B1 and PB16 occupied the ATP site and allosteric pocket of VEGFR-2 in docking studies. Conclusion: These compounds can target VEGFR-2 and are endowed with in vitro and in vivo antiangiogenic activity.
| Medienart: |
E-Artikel |
|---|
| Erscheinungsjahr: |
2021 |
|---|---|
| Erschienen: |
2021 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:13 |
|---|---|
| Enthalten in: |
Future medicinal chemistry - 13(2021), 22 vom: 19. Nov., Seite 1963-1986 |
| Sprache: |
Englisch |
|---|
| Beteiligte Personen: |
Upadhyay, Neha [VerfasserIn] |
|---|
| Links: |
|---|
| Anmerkungen: |
Date Completed 31.01.2022 Date Revised 31.01.2022 published: Print-Electronic Citation Status MEDLINE |
|---|
| doi: |
10.4155/fmc-2021-0139 |
|---|
| funding: |
|
|---|---|
| Förderinstitution / Projekttitel: |
|
| PPN (Katalog-ID): |
NLM331227770 |
|---|
| LEADER | 01000naa a22002652 4500 | ||
|---|---|---|---|
| 001 | NLM331227770 | ||
| 003 | DE-627 | ||
| 005 | 20231225213012.0 | ||
| 007 | cr uuu---uuuuu | ||
| 008 | 231225s2021 xx |||||o 00| ||eng c | ||
| 024 | 7 | |a 10.4155/fmc-2021-0139 |2 doi | |
| 028 | 5 | 2 | |a pubmed24n1104.xml |
| 035 | |a (DE-627)NLM331227770 | ||
| 035 | |a (NLM)34581188 | ||
| 040 | |a DE-627 |b ger |c DE-627 |e rakwb | ||
| 041 | |a eng | ||
| 100 | 1 | |a Upadhyay, Neha |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Development and investigation of thiazolidinedione and pyrazoline compounds as antiangiogenic weapons targeting VEGFR-2 |
| 264 | 1 | |c 2021 | |
| 336 | |a Text |b txt |2 rdacontent | ||
| 337 | |a ƒaComputermedien |b c |2 rdamedia | ||
| 338 | |a ƒa Online-Ressource |b cr |2 rdacarrier | ||
| 500 | |a Date Completed 31.01.2022 | ||
| 500 | |a Date Revised 31.01.2022 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Background: Angiogenesis deregulation is often linked to cancer and is thus an essential target. Materials & methods: Twenty-nine compounds were developed as VEGFR-2 inhibitors. Compounds were evaluated to determine their antiangiogenic activity. Results: B1, PB11 and PB16 showed HUVEC's IC50 scores in the submicromolar range. B1, B2 and PB16 reduced cellular migration and capillary tube formation of HUVECs. VEGFR-2 inhibitory activity was found in the nanomolar range: 200 nM of B1, 500 nM of B2 and 600 nM of PB16. B1 and PB16 suppressed the formation of new capillaries on growing CAMs. B1 and PB16 occupied the ATP site and allosteric pocket of VEGFR-2 in docking studies. Conclusion: These compounds can target VEGFR-2 and are endowed with in vitro and in vivo antiangiogenic activity | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Research Support, Non-U.S. Gov't | |
| 650 | 4 | |a VEGFR-2 | |
| 650 | 4 | |a antiangiogenic | |
| 650 | 4 | |a diaryl-pyrazoline | |
| 650 | 4 | |a thiazolidinedione | |
| 650 | 7 | |a Angiogenesis Inhibitors |2 NLM | |
| 650 | 7 | |a Protein Kinase Inhibitors |2 NLM | |
| 650 | 7 | |a Pyrazoles |2 NLM | |
| 650 | 7 | |a Thiazolidinediones |2 NLM | |
| 650 | 7 | |a KDR protein, human |2 NLM | |
| 650 | 7 | |a EC 2.7.10.1 |2 NLM | |
| 650 | 7 | |a Vascular Endothelial Growth Factor Receptor-2 |2 NLM | |
| 650 | 7 | |a EC 2.7.10.1 |2 NLM | |
| 700 | 1 | |a Tilekar, Kalpana |e verfasserin |4 aut | |
| 700 | 1 | |a Safuan, Sabreena |e verfasserin |4 aut | |
| 700 | 1 | |a Kumar, Alan P |e verfasserin |4 aut | |
| 700 | 1 | |a Schweipert, Markus |e verfasserin |4 aut | |
| 700 | 1 | |a Meyer-Almes, Franz-Josef |e verfasserin |4 aut | |
| 700 | 1 | |a Ramaa, C S |e verfasserin |4 aut | |
| 773 | 0 | 8 | |i Enthalten in |t Future medicinal chemistry |d 2009 |g 13(2021), 22 vom: 19. Nov., Seite 1963-1986 |w (DE-627)NLM194822109 |x 1756-8927 |7 nnns |
| 773 | 1 | 8 | |g volume:13 |g year:2021 |g number:22 |g day:19 |g month:11 |g pages:1963-1986 |
| 856 | 4 | 0 | |u http://dx.doi.org/10.4155/fmc-2021-0139 |3 Volltext |
| 912 | |a GBV_USEFLAG_A | ||
| 912 | |a GBV_NLM | ||
| 951 | |a AR | ||
| 952 | |d 13 |j 2021 |e 22 |b 19 |c 11 |h 1963-1986 | ||