Gold complexes of alkylated phosphines

Patent metadata

Field	Value
Publication number	US-10144749-B2
Application number	US-201815993163-A
Country	US
Kind code	B2
Filing date	May 30, 2018
Priority date	Apr 22, 2016
Publication date	Dec 4, 2018
Grant date	Dec 4, 2018

Abstract

Gold(I) complex with mixed ligands as an anticancer agent. The gold(I) ion is coordinated to a dithiocarbamate ligand and a phosphorus-containing ligand (e.g. phosphines). Also described are a pharmaceutical composition incorporating the gold(I) complex, a methods of synthesizing the gold(I) complex, and a method for treating cancer.

First claim

The invention claimed is:

1. A gold(I) complex represented by formula (I):

a salt thereof, a solvate thereof, or a combination thereof;
wherein R 1 and R 2 are alkyl groups independently selected from the group consisting of methyl, ethyl, and isopropyl;
R 3 , R 4 , and R 5 are independently selected from the group consisting of an optionally substituted C 1 -C 3 alkyl, an optionally substituted arylalkyl, an optionally substituted aryl, an optionally substituted vinyl, an optionally substituted alkoxy, and an optionally substituted aryloxy; and
with the proviso that R 1 , R 2 , R 3 , R 4 , and R 5 are not each an ethyl.

2. The gold(I) complex of claim 1 , wherein R 1 and R 2 are the same unsubstituted alkyl group, and R 3 , R 4 , and R 5 are the same optionally substituted C 1 -C 3 alkyl group.

3. The gold(I) complex of claim 2 , wherein R 1 and R 2 are ethyls, and R 3 , R 4 , and R 5 are methyls.

4. A composition comprising:
the gold(I) complex of claim 1 ; and
a pharmaceutically acceptable carrier or excipient.

5. The composition of claim 4 , which comprises 0.01-50 μM of the gold(I) complex relative to the total composition.

6. The composition of claim 4 , further comprising:
at least one chemotherapeutic agent selected from the group consisting of aflibercept, asparaginase, bleomycin, busulfan, carmustine, chlorambucil, cladribine, cyclophosphamide, cytarabine, dacarbazine, daunorubicin, doxorubicin, etoposide, fludarabine, gemcitabine, hydroxyurea, idarubicin, ifosfamide, irinotecan, lomustine, mechlorethamine, melphalan, mercaptopurine, methotrexate, mitomycin, mitoxantrone, pentostatin, procarbazine, topotecan, vinblastine, vincristine, retinoic acid, oxaliplatin, carboplatin, 5-fluorouracil, teniposide, amasacrine, docetaxel, paclitaxel, vinorelbine, bortezomib, clofarabine, capecitabine, actinomycin D, epirubicin, vindesine, methotrexate, 6-thioguanine, tipifarnib, imatinib, erlotinib, sorafenib, sunitinib, dasatinib, nilotinib, lapatinib, gefitinib, temsirolimus, everolimus, rapamycin, bosutinib, pzopanib, axitinib, neratinib, vatalanib, pazopanib, midostaurin, enzastaurin, trastuzumab, cetuximab, panitumumab, rituximab, bevacizumab, mapatumumab, conatumumab, and lexatumumab.

7. The gold(I) complex of claim 1 , wherein R 3 , R 4 , and R 5 are an C 1 -C 2 alkyl group.

8. The gold(I) complex of claim 1 , wherein R 1 and R 2 are the same alkyl group selected from the group consisting of a methyl group and an ethyl group, and R 3 , R 4 , and R 5 are the same alkyl group selected from the group consisting of a methyl group and an ethyl group.

9. The gold(I) complex of claim 1 , wherein R 1 and R 2 are methyls and R 3 , R 4 , and R 5 are ethyls.

Assignees

• Univ King Fahd Pet & Minerals
• Univ King Saud

Inventors

• Al-Jaroudi Said S
• Alhoshani Ali
• Altaf Muhammad
• Isab Anvarhusein Abdulkadir

Classifications

• G01N33/57515

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• A61K9/0053

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• G01N2800/52

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• A61N1/30

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