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3-[(6-Arylamino)pyridazinylamino]benzoic acids: design, synthesis and in vitro evaluation of anticancer activity
A series of novel substituted 3,6-disubstituted pyridazines based on the structure of vatalanib (PTK787) were designed and synthesized. The cytotoxicity of the final compounds was tested in vitro on HT-29 colon cancer cell line. Compounds 2a and 2b with 4-chlorophenylamino moiety, exerted the highes...
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| Published in: | Archives of pharmacal research 2013, 36(1), , pp.41-50 |
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| Main Authors: | , , , |
| Format: | Article |
| Language: | English |
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| cites | cdi_FETCH-LOGICAL-c378t-320b3aca2cf8be4d2a5ac7b807a8777600e6e49c8c9e9f680fcbd0a454abe523 |
| container_end_page | 50 |
| container_issue | 1 |
| container_start_page | 41 |
| container_title | Archives of pharmacal research |
| container_volume | 36 |
| creator | Abouzid, Khaled A. M. Khalil, Nadia A. Ahmed, Eman M. Mohamed, Khaled Omar |
| description | A series of novel substituted 3,6-disubstituted pyridazines based on the structure of vatalanib (PTK787) were designed and synthesized. The cytotoxicity of the final compounds was tested in vitro on HT-29 colon cancer cell line. Compounds
2a
and
2b
with 4-chlorophenylamino moiety, exerted the highest cytotoxic activity with IC
50
values equal to 15.3 and 3.9 μM respectively. The most promising compound,
2b
, was found to be about fivefold more active than vatalanib against HT-29 colon cancer cell line. |
| doi_str_mv | 10.1007/s12272-013-0007-8 |
| format | article |
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2a
and
2b
with 4-chlorophenylamino moiety, exerted the highest cytotoxic activity with IC
50
values equal to 15.3 and 3.9 μM respectively. The most promising compound,
2b
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2a
and
2b
with 4-chlorophenylamino moiety, exerted the highest cytotoxic activity with IC
50
values equal to 15.3 and 3.9 μM respectively. The most promising compound,
2b
, was found to be about fivefold more active than vatalanib against HT-29 colon cancer cell line.</description><subject>Antineoplastic Agents - chemical synthesis</subject><subject>Antineoplastic Agents - chemistry</subject><subject>Antineoplastic Agents - pharmacology</subject><subject>Cell Survival - drug effects</subject><subject>Drug Design</subject><subject>Drug Screening Assays, Antitumor</subject><subject>HT29 Cells</subject><subject>Humans</subject><subject>Medicine</subject><subject>Molecular Docking Simulation</subject><subject>Molecular Structure</subject><subject>Pharmacology/Toxicology</subject><subject>Pharmacy</subject><subject>Phthalazines - chemistry</subject><subject>Phthalazines - pharmacology</subject><subject>Pyridazines - chemical synthesis</subject><subject>Pyridazines - chemistry</subject><subject>Pyridazines - pharmacology</subject><subject>Pyridines - chemistry</subject><subject>Pyridines - pharmacology</subject><subject>Research Article</subject><subject>Structure-Activity Relationship</subject><subject>약학</subject><issn>0253-6269</issn><issn>1976-3786</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2013</creationdate><recordtype>article</recordtype><recordid>eNp9kU9v1DAQxS0EokvhA3BBObYShrGd2A63VcWfSpWQ0N4QsiaOs7jN2oudVEo_PS5ZOHKaGc_vPY38CHnN4B0DUO8z41xxCkxQKDPVT8iGtUpSobR8SjbAG0Ell-0ZeZHzLYCQTdM8J2dcCFA1lxtyFPT7haTbtIx48CFeHpfke3zw4fTwo3PhIXpbofV9_lD1Lvt9eFvlJUw_S58rDH3lQ3XvpxQrd4_jjJOPoYpDWU3eYrAuFfnkC7K8JM8GHLN7darnZPfp4-7qC735-vn6antDbTl-ooJDJ9Ait4PuXN1zbNCqToNCrZSSAE66urXatq4dpIbBdj1g3dTYuYaLc3K52oY0mDvrTUT_p-6juUtm-213bRgTinMo7MXKHlP8Nbs8mYPP1o0jBhfnbBjXsq1Vo0RB2YraFHNObjDH5A-YFsPAPGZi1kxMycQ8ZmJ00bw52c_dwfX_FH9DKABfgVxWYe-SuY1zCuV3_uP6GyOVmF4</recordid><startdate>2013</startdate><enddate>2013</enddate><creator>Abouzid, Khaled A. 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M.</creatorcontrib><creatorcontrib>Khalil, Nadia A.</creatorcontrib><creatorcontrib>Ahmed, Eman M.</creatorcontrib><creatorcontrib>Mohamed, Khaled Omar</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><collection>Korean Citation Index</collection><jtitle>Archives of pharmacal research</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Abouzid, Khaled A. 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2a
and
2b
with 4-chlorophenylamino moiety, exerted the highest cytotoxic activity with IC
50
values equal to 15.3 and 3.9 μM respectively. The most promising compound,
2b
, was found to be about fivefold more active than vatalanib against HT-29 colon cancer cell line.</abstract><cop>Heidelberg</cop><pub>Pharmaceutical Society of Korea</pub><pmid>23307426</pmid><doi>10.1007/s12272-013-0007-8</doi><tpages>10</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0253-6269 |
| ispartof | Archives of Pharmacal Research, 2013, 36(1), , pp.41-50 |
| issn | 0253-6269 1976-3786 |
| language | eng |
| recordid | cdi_nrf_kci_oai_kci_go_kr_ARTI_1137220 |
| source | Springer Link |
| subjects | Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Cell Survival - drug effects Drug Design Drug Screening Assays, Antitumor HT29 Cells Humans Medicine Molecular Docking Simulation Molecular Structure Pharmacology/Toxicology Pharmacy Phthalazines - chemistry Phthalazines - pharmacology Pyridazines - chemical synthesis Pyridazines - chemistry Pyridazines - pharmacology Pyridines - chemistry Pyridines - pharmacology Research Article Structure-Activity Relationship 약학 |
| title | 3-[(6-Arylamino)pyridazinylamino]benzoic acids: design, synthesis and in vitro evaluation of anticancer activity |
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