| dc.identifier.uri | http://hdl.handle.net/11401/77101 | |
| dc.description.sponsorship | This work is sponsored by the Stony Brook University Graduate School in compliance with the requirements for completion of degree. | en_US |
| dc.format | Monograph | |
| dc.format.medium | Electronic Resource | en_US |
| dc.language.iso | en_US | |
| dc.publisher | The Graduate School, Stony Brook University: Stony Brook, NY. | |
| dc.type | Thesis | |
| dcterms.abstract | Cancer is a group of diseases characterized by uncontrolled growth and spread of abnormal cells, and it is the leading cause of death around the world. Despite of great advance made in the medical research, there is no universal treatment for cancer. Chemotherapy is advantageous and widely used because it is not invasive, and there are many different chemotherapeutic agents to different cancers. Chemotherapy relies on the premise that rapid dividing cells are more likely to be attacked by cytotoxic agents. Paclitaxel (Taxol) is a mitotic inhibitor used in cancer chemotherapy and is one of the most effective antitumor drugs available for various cancers, such as ovarian cancer, breast cancer, and AIDS-related Kaposi's sarcoma. Its analogues docetaxel (Taxotere®) and cabazitaxel (Jevtana®) are also chemotherapeutic agents for breast cancer and prostate cancer respectively. Taxoids can be accessed through modified 10-DAB III intermediate coupled with enantiopure β -lactam via Ojima-Holton coupling to afford the taxoids. Using this coupling method, new generation of taxoids have been synthetized effectively. Lack of tumor specificity is the main challenges which cause undesired side effects of chemotherapy. In last few decades, various drug delivery protocol and systems have been explored. In general, tumor-targeting drug-delivery system consists of a cytotoxic agent and a tumor-targeting moiety which can be linked directly or bridged by a suitable linker to form a conjugate. The conjugate should be systemically non-toxic, stable in circulation, and delivered to tumor cells specifically. As the tumor-targeting moiety (TTM) is recognized by receptors of the tumor cells, the conjugate can be internalized into the cells and cleaved to regenerate the active cytotoxic agent. Ojima group has constructed many tumor-targeting drug-delivery systems; one of the examples is using biotin (vitamin B) as tumor targeting moiety, new-generation taxoid (SB-T-1214) as cytotoxic agent, and they are bound together by methyl-branch disulfide linker. The syntheses of these drug conjugates will be discussed. | |
| dcterms.abstract | Cancer is a group of diseases characterized by uncontrolled growth and spread of abnormal cells, and it is the leading cause of death around the world. Despite of great advance made in the medical research, there is no universal treatment for cancer. Chemotherapy is advantageous and widely used because it is not invasive, and there are many different chemotherapeutic agents to different cancers. Chemotherapy relies on the premise that rapid dividing cells are more likely to be attacked by cytotoxic agents. Paclitaxel (Taxol) is a mitotic inhibitor used in cancer chemotherapy and is one of the most effective antitumor drugs available for various cancers, such as ovarian cancer, breast cancer, and AIDS-related Kaposi's sarcoma. Its analogues docetaxel (Taxotere®) and cabazitaxel (Jevtana®) are also chemotherapeutic agents for breast cancer and prostate cancer respectively. Taxoids can be accessed through modified 10-DAB III intermediate coupled with enantiopure β -lactam via Ojima-Holton coupling to afford the taxoids. Using this coupling method, new generation of taxoids have been synthetized effectively. Lack of tumor specificity is the main challenges which cause undesired side effects of chemotherapy. In last few decades, various drug delivery protocol and systems have been explored. In general, tumor-targeting drug-delivery system consists of a cytotoxic agent and a tumor-targeting moiety which can be linked directly or bridged by a suitable linker to form a conjugate. The conjugate should be systemically non-toxic, stable in circulation, and delivered to tumor cells specifically. As the tumor-targeting moiety (TTM) is recognized by receptors of the tumor cells, the conjugate can be internalized into the cells and cleaved to regenerate the active cytotoxic agent. Ojima group has constructed many tumor-targeting drug-delivery systems; one of the examples is using biotin (vitamin B) as tumor targeting moiety, new-generation taxoid (SB-T-1214) as cytotoxic agent, and they are bound together by methyl-branch disulfide linker. The syntheses of these drug conjugates will be discussed. | |
| dcterms.available | 2017-09-20T16:51:57Z | |
| dcterms.contributor | Ojima, Iwao | en_US |
| dcterms.creator | Chen, Ying-Jen | |
| dcterms.dateAccepted | 2017-09-20T16:51:57Z | |
| dcterms.dateSubmitted | 2017-09-20T16:51:57Z | |
| dcterms.description | Department of Chemistry. | en_US |
| dcterms.extent | 153 pg. | en_US |
| dcterms.format | Monograph | |
| dcterms.format | Application/PDF | en_US |
| dcterms.identifier | http://hdl.handle.net/11401/77101 | |
| dcterms.issued | 2015-08-01 | |
| dcterms.language | en_US | |
| dcterms.provenance | Made available in DSpace on 2017-09-20T16:51:57Z (GMT). No. of bitstreams: 1
Chen_grad.sunysb_0771M_11548.pdf: 12516195 bytes, checksum: b9ce1a24360320d445f43ecd36412d14 (MD5)
Previous issue date: 2013 | en |
| dcterms.publisher | The Graduate School, Stony Brook University: Stony Brook, NY. | |
| dcterms.subject | Chemistry | |
| dcterms.title | Synthesis of New-Generation Taxoid and Taxoid-Based Tumor-Targeting Drug Conjugates | |
| dcterms.type | Thesis | |
