Design, Synthesis, Molecular Modelling and Anticancer Activities of New Fused Phenanthrolines
Three series of fused pyrrolophenanthroline derivatives were designed as analogues of phenstatin and synthesized in two steps starting with 1,7-phenanthroline, 4,7-phenanthroline and 1,10-phenanthroline, respectively. Two (Compounds 8a and 11c) of the four compounds tested against a panel of sixty human cancer cell lines of the National Cancer Institute (NCI) exhibited significant growth inhibition activity on several cell lines. Compound 11c showed a broad spectrum in terms of antiproliferative efficacy with GI50 values in the range of 0.296 to 250 μM. Molecular docking studies indicated that Compounds 8a and 11c are accommodated in the colchicine binding site of tubulin in two different ways.
| Medienart: |
E-Artikel |
|---|
| Erscheinungsjahr: |
2020 |
|---|---|
| Erschienen: |
2020 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:25 |
|---|---|
| Enthalten in: |
Molecules (Basel, Switzerland) - 25(2020), 3 vom: 25. Jan. |
| Sprache: |
Englisch |
|---|
| Beteiligte Personen: |
Al Matarneh, Cristina Maria [VerfasserIn] |
|---|
| Links: |
|---|
| Themen: |
3 + 2 cycloaddition |
|---|
| Anmerkungen: |
Date Completed 11.11.2020 Date Revised 11.11.2020 published: Electronic Citation Status MEDLINE |
|---|
| doi: |
10.3390/molecules25030527 |
|---|
| funding: |
|
|---|---|
| Förderinstitution / Projekttitel: |
|
| PPN (Katalog-ID): |
NLM305878913 |
|---|
| LEADER | 01000naa a22002652 4500 | ||
|---|---|---|---|
| 001 | NLM305878913 | ||
| 003 | DE-627 | ||
| 005 | 20231225122130.0 | ||
| 007 | cr uuu---uuuuu | ||
| 008 | 231225s2020 xx |||||o 00| ||eng c | ||
| 024 | 7 | |a 10.3390/molecules25030527 |2 doi | |
| 028 | 5 | 2 | |a pubmed24n1019.xml |
| 035 | |a (DE-627)NLM305878913 | ||
| 035 | |a (NLM)31991806 | ||
| 035 | |a (PII)E527 | ||
| 040 | |a DE-627 |b ger |c DE-627 |e rakwb | ||
| 041 | |a eng | ||
| 100 | 1 | |a Al Matarneh, Cristina Maria |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Design, Synthesis, Molecular Modelling and Anticancer Activities of New Fused Phenanthrolines |
| 264 | 1 | |c 2020 | |
| 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 11.11.2020 | ||
| 500 | |a Date Revised 11.11.2020 | ||
| 500 | |a published: Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Three series of fused pyrrolophenanthroline derivatives were designed as analogues of phenstatin and synthesized in two steps starting with 1,7-phenanthroline, 4,7-phenanthroline and 1,10-phenanthroline, respectively. Two (Compounds 8a and 11c) of the four compounds tested against a panel of sixty human cancer cell lines of the National Cancer Institute (NCI) exhibited significant growth inhibition activity on several cell lines. Compound 11c showed a broad spectrum in terms of antiproliferative efficacy with GI50 values in the range of 0.296 to 250 μM. Molecular docking studies indicated that Compounds 8a and 11c are accommodated in the colchicine binding site of tubulin in two different ways | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a 3 + 2 cycloaddition | |
| 650 | 4 | |a anticancer | |
| 650 | 4 | |a phenanthrolines | |
| 650 | 4 | |a phenstatin | |
| 650 | 4 | |a tubulin docking | |
| 650 | 7 | |a Antineoplastic Agents |2 NLM | |
| 650 | 7 | |a Phenanthrolines |2 NLM | |
| 700 | 1 | |a Amarandi, Roxana Maria |e verfasserin |4 aut | |
| 700 | 1 | |a Craciun, Anda Mihaela |e verfasserin |4 aut | |
| 700 | 1 | |a Mangalagiu, Ionel I |e verfasserin |4 aut | |
| 700 | 1 | |a Zbancioc, Gheorghita |e verfasserin |4 aut | |
| 700 | 1 | |a Danac, Ramona |e verfasserin |4 aut | |
| 773 | 0 | 8 | |i Enthalten in |t Molecules (Basel, Switzerland) |d 2004 |g 25(2020), 3 vom: 25. Jan. |w (DE-627)NLM172073448 |x 1420-3049 |7 nnns |
| 773 | 1 | 8 | |g volume:25 |g year:2020 |g number:3 |g day:25 |g month:01 |
| 856 | 4 | 0 | |u http://dx.doi.org/10.3390/molecules25030527 |3 Volltext |
| 912 | |a GBV_USEFLAG_A | ||
| 912 | |a GBV_NLM | ||
| 951 | |a AR | ||
| 952 | |d 25 |j 2020 |e 3 |b 25 |c 01 | ||